Chrysin, as a flavone, is a promising drug candidate because of its multifaceted properties, such as anti-inflammatory, antioxidant and anticancer. However, its poor bioavailability is a bottleneck for pharmaceutical applications. To enhance the bioactive effects, chrysin-loaded poly (D,L-lactic-co-glycolic acid) and polyvinyl alcohol were successfully prepared to overcome problems associated with chrysin. The properties of modified nanochrysin were analysed by in vitro dissolution study, XRD, FTIR and SEM. Free radical scavenging potentials of the modified nanochrysin against DPPH were confirmed based on its stable antioxidant effects. A DNA instability enhancement was observed after HO exposure, whereas chrysin decreased the HO activity, and modified nanochrysin was more potent in this regard. Blood compatibility on red blood cells was confirmed by haemolytic and in vitro cytotoxicity assays. The in vitro anticancer activity of the modified nanochrysin towards MCF-7 and SKOV-3 cell lines using various parameters was investigated. The nanochrysin was found to exert cell growth arrest against both cancer cells in a dose-dependent manner. IC value was significantly decreased in nanochrysin in comparison with pure chrysin and induced apoptotic cell death pathway. The results of this study suggest that the nanochrysin might be used for medical applications and offer a beneficial formulation for chemotherapy.

Hesperidin, as a flavonone, is recognized as promising anti-inflammatory, antioxidant, and anticancer agent. Its poor bioavailability is crucial bottleneck for therapeutic efficacy. To enhance the stability and bioactive potentials, hesperidin-PLGA-Poloxamer 407 was successfully prepared to minimize or overcome problems associated with hesperidin absorption. The characteristics of nanohesperidin were testing by in vitro dissolution study, XRD, FTIR, PSA and SEM. Antioxidant effects of nanohesperidin were studied. The structure-activity relationship analysis with antioxidant pharmacophore has been performed by using density functional theory method and quantum chemical calculations. The structural properties were investigated using Becke three-parameter hybrid exchange and the Lee-Yang-Parr correction functional methods. Nanohesperidin was found to decrease the H 2 O 2 activity-induced DNA instability. Blood compatibility on human erythrocytes was confirmed by haemolytic and in vitro toxicity assessments. The in vitro anticancer activity of nanohesperidin towards MCF-7 cells using various parameters was carried out. The nanohesperidin was found to exert cell growth arrest, activated DNA fragmentation and induced apoptotic cell death through caspase-3 and p53-dependent pathways. These findings showed that nanohesperidin play an important role in its anticancer effects, suggesting might be used for clinical trials and can represent driving formulation for novel chemotherapeutic agents.

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